Abstract: An object of the present invention is to provide an ?,?-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like. The ?,?-unsaturated amide compound represented by the following formula (I) or a pharmaceutically acceptable salt or the like thereof has anticancer activity and the like: [wherein, “A” represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO2—, —NRX1— (wherein, RX1 represents hydrogen atom or lower alkyl), —CHRX2— (wherein, RX2 represents hydrogen atom or hydroxy), —CH?CH—, ?CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

Abstract: The invention relates to an antibody which binds to cell adhesion molecule 3 (CADM3) or an antibody fragment thereof, a hybridoma which produces the antibody or the antibody fragment thereof, a nucleic acid comprising a nucleotide sequence encoding the antibody or the antibody fragment thereof, a transformant cell comprising a vector comprising the nucleic acid, a method for producing the antibody or the antibody fragment thereof, a composition comprising the antibody or the antibody fragment thereof, and a method for detecting or measuring an antigen present in the brain, a method for diagnosing or treating a brain disease, a method for enhancing the property of accumulating in a brain of an antibody, and a method for increasing the amount of an antibody in the brain, each of which using the antibody or the antibody fragment thereof, and the like.

Abstract: The object of the present invention is to provide a therapeutic agent for hyperphosphatemia capable sufficiently decreasing a serum phosphorus concentration with a small dose, and particles therefor. The present invention provides a therapeutic agent for hyperphosphatemia, which comprises, as an active ingredient, a particle containing a crosslinked polymer having a substituent containing a NRA1RA2 structure or a salt thereof, wherein the particle has an average particle diameter of 20 to 150 ?m and a swelling rate of 9 to 16 mL/g (wherein RA1 and RA2 each independently represent a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, an aminoalkyl group having 1 to 20 carbon atoms or a salt thereof, or the like).

Abstract: An object of the present invention is to provide an anti-BMP10 antibody, and a therapeutic agent for hypertension and a hypertensive disease, containing the antibody as an active ingredient. The present invention relates to an anti-BMP10 monoclonal antibody or an antibody fragment thereof that binds to human BMP10 (bone morphogenetic protein 10). Further, the present invention relates to a therapeutic agent for hypertension and a hypertensive disease containing an antagonist for at least one of BMP10 and a BMP9/BMP10 heterodimer, a diagnostic agent or a pharmaceutical composition for a disease associated with human BMP10, an immunological detection method or a measurement method for human BMP10 using the antagonist, and use of the antagonist for producing a pharmaceutical composition for treating hypertension and a hypertensive disease.

Abstract: The present invention relates to a monoclonal antibody or antibody fragment thereof as a human IgG antibody including at least one lysine derivative in a constant region of the human IgG antibody; a modified antibody or antibody fragment thereof, wherein the lysine derivative is modified; a nucleic acid including a nucleotide sequence encoding the antibody or antibody fragment thereof; a vector including the nucleic acid; a transformed cell obtained by introducing the vector into a host cell; a method for producing the antibody or antibody fragment thereof; and a composition containing the antibody or antibody fragment thereof.

Abstract: The present invention provides, for example, an oligonucleotide derivative or a salt thereof comprising a circular oligonucleotide and a linear oligonucleotide, wherein the circular oligonucleotide and the linear oligonucleotide have base sequences complementary to each other, and form a complex via a hydrogen bond between the complementary base sequences, and a method for producing the same.

Abstract: The present invention relates to a therapeutic agent for an ophthalmic disease comprising a vascular endothelial growth factor (VEGF) receptor inhibitor or an epidermal growth factor (EGF) receptor inhibitor in a nanoparticle form, having a property to be retained in a posterior eye tissue when systemically administered.

Abstract: An object of the present invention is to provide a novel IL-2 variant which has improved selectivity for IL-2R??? and selectively activates Tregs. The present invention relates to an IL-2 variant, a method for producing the IL-2 variant, a composition and a therapeutic agent for an immune disease, comprising the IL-2 variant, a method for increasing selectivity of IL-2 for IL-2R???, a method for improving an affinity of IL-2 for an IL-2R? subunit, a method of reducing an affinity of IL-2 for at least one of an IL-2R? subunit and an IL-2R? subunit, and a method for selectively activating regulatory T cells.

Abstract: The present invention relates to a monoclonal antibody or antibody fragment thereof as a human IgG antibody including at least one lysine derivative in a constant region of the human IgG antibody; a modified antibody or antibody fragment thereof, wherein the lysine derivative is modified; a nucleic acid including a nucleotide sequence encoding the antibody or antibody fragment thereof; a vector including the nucleic acid; a transformed cell obtained by introducing the vector into a host cell; a method for producing the antibody or antibody fragment thereof; and a composition containing the antibody or antibody fragment thereof.

Abstract: A compound having anticancer activity, or a pharmaceutically acceptable salt thereof is provided. Used is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: (wherein, L1 and L2 are the same or different and each represents a group represented by one formula selected from the group consisting of formulas (A) to (F), and S represents a group represented by one formula selected from the group consisting of formulas (S1) to (S18)).

Abstract: The present invention relates to a therapeutic agent for an ophthalmic disease comprising a vascular endothelial growth factor (VEGF) receptor inhibitor or an epidermal growth factor (EGF) receptor inhibitor in a nanoparticle form, having a property to be retained in a posterior eye tissue when systemically administered.

Abstract: Provided is a production method of a thiazole derivative represented by the formula (I), which has an adenosine A2A receptor antagonistic action and is useful as a therapeutic agent for, for example, Parkinson's disease, sleep disorder, analgesic resistance to opioid, migraine, movement disorder, depression, anxiety disorder and the like. Also provided is a production method of a compound represented by the formula (C), which contains (i) a step of reacting a compound represented by the formula (A) and a compound represented by the formula (B), and the like: (wherein R1 represents furyl, R4, R5 and R6 are the same or different and each represents lower alkyl or aryl, R2 represents pyridyl or tetrahydropyranyl, and X1 represents halogen).

Abstract: The present invention provides a nucleic acid-containing lipid nanoparticle comprising an analog of a fatty acid ester of glycerol, and a nucleic acid, wherein the analog is not hydrolyzable by a lipase.

Abstract: The present invention provides a method for producing a pharmaceutical composition containing fine particles of a poorly soluble drug, comprising mixing a sugar or a sugar alcohol with a dispersion of nanoparticles of the poorly soluble drug and granulating the obtained mixture.

Abstract: The present invention provides an ?,?-unsaturated amide compound or a pharmaceutically acceptable salt or the like thereof having anticancer activity and the like represented by the following formula (I): [wherein, “A” represents optionally substituted heterocyclic diyl, R1 represents hydrogen atom or optionally substituted lower alkyl, R2 represents optionally substituted aryl, optionally substituted cycloalkyl, optionally substituted aliphatic heterocyclic group or optionally substituted aromatic heterocyclic group, X represents —O—, —S—, —SO2—, —NRX1— (wherein, RX1 represents hydrogen atom or lower alkyl), —CHRX2— (wherein, RX2 represents hydrogen atom or hydroxy), —CH?CH—, —CO— or —NH—CO—, and n1 and n2 are the same or different, and each represents 0 or 1].

Abstract: The present invention relates to a nucleic acid conjugate represented by the following formula 1: wherein X is an oligonucleotide, L1 and L2 are each independently sugar ligand, and S1, S2 and S3 are each independently a linker.

Abstract: An object of the present invention is to provide a monoclonal antibody which binds to a human CC chemokine receptor 1 (CCR1) and inhibits activation of the human CCR1, or an antibody fragment thereof. The present invention relates to a monoclonal antibody which binds to an extracellular region of a human CCR1 and inhibits activation of the human CCR1 by a human CC chemokine ligand 15 (CCL15), or an antibody fragment thereof, a hybridoma producing the antibody, a nucleic acid having a nucleotide sequence encoding the antibody or the antibody fragment, a transformant cell containing a vector containing the nucleic acid, a method for producing the antibody or the antibody fragment using the hybridoma or the transformant cell; a therapeutic agent and a diagnostic agent containing the antibody or the antibody fragment, and a method for treating and diagnosing a CCR1-related disease using the antibody or the antibody fragment.

Abstract: The present invention provides a double-stranded nucleic acid consisting of a sense-strand nucleic acid and an antisense-strand nucleic acid and comprising a double-strand region having at least 11 base pairs, for suppressing expression of APCS gene, in which an oligonucleotide chain having a chain length of at least 17 nucleotides and at most 30 nucleotides in the antisense-strand nucleic acid is complementary to a target APCS mRNA sequence comprising a base sequence set forth in any one of SEQ ID NOS: 1288 to 1930.

Abstract: The present invention provides a nitrogen-containing heterocyclic compound or a pharmaceutically acceptable salt thereof having an inhibitory effect on the production of kynurenine, represented by formula (I): (wherein R6 and R7 may be the same or different and each represent a hydrogen atom or the like, R8, R9, R10, and R11 may be the same or different and each represent a hydrogen atom or the like, R1 represents lower alkyl which may be substituted with cycloalkyl, or the like, and R3 represents optionally substituted aryl or an optionally substituted heterocyclic group).

Abstract: An object of the present invention is to provide a method of enabling efficient structural analysis of a target protein that has been impossible or difficult to analyze so far, by stabilizing the target protein. The present invention provides an anti-BRIL antibody which specifically binds to BRIL or a BRIL fusion protein and an antigen-binding fragment thereof, a nucleic acid encoding the anti-BRIL antibody and the antigen-binding fragment thereof, a vector containing the nucleic acid, an antibody producing cell containing the vector, a method of producing the antibody, and a method of using the antibody in a protein structural analysis.